Rho
Rho产品
目录号 | 产品描述 | 文献引用 | 实验数据 |
---|---|---|---|
S1573 |
Fasudil (HA-1077) HClFasudil(HA-1077)是一种有效的、具有选择性的Rho抑制剂(ROCK2, Ki=0.33 μM),同时对PKA、PKG、PKC和MLCK也具有抑制活性,Ki值分别为1.6 μM、1.6 μM、3.3 μM、36 μM。Fasudil 也是calcium channel的阻滞剂。 |
![]() ![]() The ROCK inhibitors fasudil and Y27632 prevented SCP2 cell bone metastasis in nude mice (n = 10 per group). Shown are BLI images of bone metastases, IHC analyses of SMAD3 C-tail phosphorylation and PTHLH, osteoclast TRAP staining, and BLI quantitation. |
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S1314 |
Zoledronic AcidZoledronic acid (ZA, Zoledronate, CGP-4244), 破骨细胞抑制剂,通过抑制甲羟戊酸途径诱导破骨细胞凋亡,并防止小GTP结合蛋白,如Ras 和 Rho的异戊二烯化。Zoledronic acid (ZA) 还可诱导自噬。 |
![]() ![]() Isolation of cd T cells. PBMCs were cultured in the presence of 400 nM ZA and 200 IU/ml IL-2 over 10 days. cd T cells were isolated by negative MACS isolation. Flow cytometric analysis revealed co-expression of CD3 and TCRcd on over 99% of cells of the flow through fraction (A). The T cells expressed the TCRVd2 chain (B) and the CD56 protein (C).
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S8031 |
NSC 23766NSC 23766是一种Rac GTPase抑制剂,通过鸟嘌呤核苷酸因子(GEFs)靶向作用于Rac 活化,无细胞试验中IC50为~50 μM;但是不会抑制密切相关的靶点,Cdc42或RhoA。 |
![]() ![]() MES cells were treated with Rac inhibitor (50 μM EHT1864 or NSC23766) and assayed for self-renewal by serial passage mammosphere formation. P1, passage 1; P2, passage 2. Data are means ± SEM of three biological replicates. *P ≤ 0.05 by two-tailed t test.
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S7319 |
EHop-016EHop-016 是一种特异性Rac GTPase抑制剂,在MDA-MB-435 和 MDA-MB-231细胞中作用于Rac1,IC50为1.1 μM,同等有效抑制Rac3。 |
![]() ![]() (f) Liver samples from both groups treated with olive oil, CCl4, CCl4+NSC23766 or +EHop-016 for 4 weeks were collected for Rac1 activity assay and western blot analysis. |
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S1721 |
AzathioprineAzathioprine 是一种抑制免疫系统的药物,抑制了嘌呤的合成以及GTP结合蛋白Rac1的激活,用于器官移植和自身免疫性疾病。 |
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S3239New |
Emetine DihydrochlorideEmetine Dihydrochloride 是一种从吐根 ipecac 根部提取的主要生物碱,在临床上被用作催吐和抗原生动物药物,可降低 HIFs (hypoxia-inducible factors; HIF-1α and HIF-2α)、PDK1、RhoA、Rho-kinases (ROCK1 and ROCK2) 和 BRD4。Emetine Dihydrochloride 可抑制细胞的自噬,并具有抗疟疾、抗病毒、抗细菌和抗变形虫的作用。 已取得危险化学品经营许可 |
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S0890New |
MLS000532223MLS000532223 是一种 Rho family GTPases 的高亲和力的选择性抑制剂,EC50值为16 μM至120 μM。 |
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S6673New |
CCG-222740CCG-222740是一种Rho/MRTF通路抑制剂。CCG-222740通过降低α平滑肌肌动蛋白(α-SMA)的表达水平来降低星状细胞在体外和体内的活化。 |
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S7293 |
ZCL278ZCL278是一个选择性的Cdc42 GTP酶抑制剂,Kd为11.4 μM。 |
![]() ![]() Rho GTPases were involved in NaAsO2 induced apoptosis in rat CGNs. A. Representative fluorescence images of cells exposed to 0 and 10 μM NaAsO2 for 24 h with or without ZCL278 (an inhibitor of Cdc42), or a Rac1 inhibitor NSC23766. Both ZCL278 and NSC23766 reduced the apoptotic cells. B. The graph indicates TUNEL-positive rat CGNs exposed to NaAsO2 (10 μM) with ZCL278 or NSC23766 groups decreased significantly compared with those of NaAsO2 treatment group. Data are expressed as mean ± SD from at least 5 visual fields. C. Rat CGNs in 96-well plates were treated by 0 and 10 μM NaAsO2 for 24h with or without ZCL278 (an inhibitor of Cdc42) pretreatment for 1 h, or a Rac1 inhibitor NSC23766 pretreatment for 12 h, and assessed by a CCK-8. ZCL278 and NSC23766 increased rat CGNs viability exposed to NaAsO2. All statistical results are expressed as means±SD from at least three independent experiments. ***P<0.001 vs control, # P<0.05, ##P<0.01, ###P<0.001 VS NaAsO2 treatment group. |
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S8749 |
MBQ-167MBQ-167是一种有效的Rac和Cdc42双重抑制剂,在转移性乳腺癌细胞中,IC50分别为103 nM和78 nM。 |
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S7719 |
CCG-1423CCG-1423是一种特定的 RhoA 通路抑制剂,能够抑制SRF介导的转录。 |
![]() ![]() Cells were treated with CCG-1423 for 48 h. CCG-1423 blocked the nuclear translocation of MRTF-A.
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S8469 |
CCG-203971CCG-203971是一种新型的Rho/MRTF/SRF通路抑制剂,对SRE.L.的IC50值为0.64 μM。它可以抑制Rho介导的基因转录。 |
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S7482 |
EHT 1864 2HClEHT 1864 2HCl是一种强效的Rac family GTPase抑制剂,其对Rac1, Rac1b, Rac2 和 Rac3的Kd分别为40 nM, 50 nM, 60 nM 和 250 nM 。 |
![]() ![]() E) Representative images of 3-dimensional visualization of vessel networks, H&E staining, and Masson staining. Dotted straight line indicates the femur—implant junction (F, femur; I, implant). Black box, implant region; blue arrows, osteocytes; yellow arrows, osteoblast cells; black triangle, newly formed bone or implant debris, black arrows, chondrocyte-like cells; red triangle, blood sinus. Scale bars, 200 μm.
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S7686 |
ML141ML141 (CID-2950007) 是 Rho 家族GTPase cdc42的一种有效的,选择性可逆非竞争性抑制剂,IC50为200 nM。对cdc42比对其他Rho家族中的GTPases(如Rac1, Rab2, Rab7)更有选择性。 ML141 与 p38 激活增加有关,并可能诱导p38依赖性凋亡/衰老。ML141还可保护神经母细胞瘤细胞免受二甲双胍(metformin)诱导的凋亡。 |
![]() ![]() (A) The survival rate detected at 72 h after the injection of different concentrations of ML141; shrimp injected with DMSO were used as controls. (B) The expression of WSSV IE1 at the mRNA level at 24 h post ML141 injection. Shrimp injected with the same amount of DMSO in each group were used as controls.
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S5244 |
Zoledronic acid monohydrateZoledronic acid (Zoledronate, CGP-4244) monohydrate 是 Zoledronic acid (唑来膦酸) 的一水合物,是有效的破骨细胞抑制剂,可通过抑制甲戊二羟酸途径的酶、阻止小GTP结合蛋白如Ras和Rho的异戊二烯化来诱导破骨细胞凋亡。 |
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S6752 |
Y16Y16是G蛋白偶联Rho GEFs抑制剂。它能阻止LARG和Rho的结合,Kd值为80 nM。 |
||
S0765New |
MAZ51MAZ51 是一种选择性的 vascular endothelial growth factor receptor (VEGFR)-3 (Flt-4) tyrosine kinase 的有效抑制剂。MAZ51 通过 Akt/GSK3β 的磷酸化和 RhoA 的激活来诱导神经胶质瘤细胞的细胞圆缩和G2/M细胞周期停滞。 MAZ51 可抑制多种非VEGFR-3表达肿瘤细胞的增殖并诱导其凋亡。 |
目录号 | 产品描述 | 文献引用 | 实验数据 |
---|---|---|---|
S1573 |
Fasudil (HA-1077) HClFasudil(HA-1077)是一种有效的、具有选择性的Rho抑制剂(ROCK2, Ki=0.33 μM),同时对PKA、PKG、PKC和MLCK也具有抑制活性,Ki值分别为1.6 μM、1.6 μM、3.3 μM、36 μM。Fasudil 也是calcium channel的阻滞剂。 |
![]() ![]() The ROCK inhibitors fasudil and Y27632 prevented SCP2 cell bone metastasis in nude mice (n = 10 per group). Shown are BLI images of bone metastases, IHC analyses of SMAD3 C-tail phosphorylation and PTHLH, osteoclast TRAP staining, and BLI quantitation. |
|
S1314 |
Zoledronic AcidZoledronic acid (ZA, Zoledronate, CGP-4244), 破骨细胞抑制剂,通过抑制甲羟戊酸途径诱导破骨细胞凋亡,并防止小GTP结合蛋白,如Ras 和 Rho的异戊二烯化。Zoledronic acid (ZA) 还可诱导自噬。 |
![]() ![]() Isolation of cd T cells. PBMCs were cultured in the presence of 400 nM ZA and 200 IU/ml IL-2 over 10 days. cd T cells were isolated by negative MACS isolation. Flow cytometric analysis revealed co-expression of CD3 and TCRcd on over 99% of cells of the flow through fraction (A). The T cells expressed the TCRVd2 chain (B) and the CD56 protein (C).
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S8031 |
NSC 23766NSC 23766是一种Rac GTPase抑制剂,通过鸟嘌呤核苷酸因子(GEFs)靶向作用于Rac 活化,无细胞试验中IC50为~50 μM;但是不会抑制密切相关的靶点,Cdc42或RhoA。 |
![]() ![]() MES cells were treated with Rac inhibitor (50 μM EHT1864 or NSC23766) and assayed for self-renewal by serial passage mammosphere formation. P1, passage 1; P2, passage 2. Data are means ± SEM of three biological replicates. *P ≤ 0.05 by two-tailed t test.
|
|
S7319 |
EHop-016EHop-016 是一种特异性Rac GTPase抑制剂,在MDA-MB-435 和 MDA-MB-231细胞中作用于Rac1,IC50为1.1 μM,同等有效抑制Rac3。 |
![]() ![]() (f) Liver samples from both groups treated with olive oil, CCl4, CCl4+NSC23766 or +EHop-016 for 4 weeks were collected for Rac1 activity assay and western blot analysis. |
|
S1721 |
AzathioprineAzathioprine 是一种抑制免疫系统的药物,抑制了嘌呤的合成以及GTP结合蛋白Rac1的激活,用于器官移植和自身免疫性疾病。 |
||
S3239New |
Emetine DihydrochlorideEmetine Dihydrochloride 是一种从吐根 ipecac 根部提取的主要生物碱,在临床上被用作催吐和抗原生动物药物,可降低 HIFs (hypoxia-inducible factors; HIF-1α and HIF-2α)、PDK1、RhoA、Rho-kinases (ROCK1 and ROCK2) 和 BRD4。Emetine Dihydrochloride 可抑制细胞的自噬,并具有抗疟疾、抗病毒、抗细菌和抗变形虫的作用。 已取得危险化学品经营许可 |
||
S0890New |
MLS000532223MLS000532223 是一种 Rho family GTPases 的高亲和力的选择性抑制剂,EC50值为16 μM至120 μM。 |
||
S6673New |
CCG-222740CCG-222740是一种Rho/MRTF通路抑制剂。CCG-222740通过降低α平滑肌肌动蛋白(α-SMA)的表达水平来降低星状细胞在体外和体内的活化。 |
||
S7293 |
ZCL278ZCL278是一个选择性的Cdc42 GTP酶抑制剂,Kd为11.4 μM。 |
![]() ![]() Rho GTPases were involved in NaAsO2 induced apoptosis in rat CGNs. A. Representative fluorescence images of cells exposed to 0 and 10 μM NaAsO2 for 24 h with or without ZCL278 (an inhibitor of Cdc42), or a Rac1 inhibitor NSC23766. Both ZCL278 and NSC23766 reduced the apoptotic cells. B. The graph indicates TUNEL-positive rat CGNs exposed to NaAsO2 (10 μM) with ZCL278 or NSC23766 groups decreased significantly compared with those of NaAsO2 treatment group. Data are expressed as mean ± SD from at least 5 visual fields. C. Rat CGNs in 96-well plates were treated by 0 and 10 μM NaAsO2 for 24h with or without ZCL278 (an inhibitor of Cdc42) pretreatment for 1 h, or a Rac1 inhibitor NSC23766 pretreatment for 12 h, and assessed by a CCK-8. ZCL278 and NSC23766 increased rat CGNs viability exposed to NaAsO2. All statistical results are expressed as means±SD from at least three independent experiments. ***P<0.001 vs control, # P<0.05, ##P<0.01, ###P<0.001 VS NaAsO2 treatment group. |
|
S8749 |
MBQ-167MBQ-167是一种有效的Rac和Cdc42双重抑制剂,在转移性乳腺癌细胞中,IC50分别为103 nM和78 nM。 |
||
S7719 |
CCG-1423CCG-1423是一种特定的 RhoA 通路抑制剂,能够抑制SRF介导的转录。 |
![]() ![]() Cells were treated with CCG-1423 for 48 h. CCG-1423 blocked the nuclear translocation of MRTF-A.
|
|
S8469 |
CCG-203971CCG-203971是一种新型的Rho/MRTF/SRF通路抑制剂,对SRE.L.的IC50值为0.64 μM。它可以抑制Rho介导的基因转录。 |
||
S7482 |
EHT 1864 2HClEHT 1864 2HCl是一种强效的Rac family GTPase抑制剂,其对Rac1, Rac1b, Rac2 和 Rac3的Kd分别为40 nM, 50 nM, 60 nM 和 250 nM 。 |
![]() ![]() E) Representative images of 3-dimensional visualization of vessel networks, H&E staining, and Masson staining. Dotted straight line indicates the femur—implant junction (F, femur; I, implant). Black box, implant region; blue arrows, osteocytes; yellow arrows, osteoblast cells; black triangle, newly formed bone or implant debris, black arrows, chondrocyte-like cells; red triangle, blood sinus. Scale bars, 200 μm.
|
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S7686 |
ML141ML141 (CID-2950007) 是 Rho 家族GTPase cdc42的一种有效的,选择性可逆非竞争性抑制剂,IC50为200 nM。对cdc42比对其他Rho家族中的GTPases(如Rac1, Rab2, Rab7)更有选择性。 ML141 与 p38 激活增加有关,并可能诱导p38依赖性凋亡/衰老。ML141还可保护神经母细胞瘤细胞免受二甲双胍(metformin)诱导的凋亡。 |
![]() ![]() (A) The survival rate detected at 72 h after the injection of different concentrations of ML141; shrimp injected with DMSO were used as controls. (B) The expression of WSSV IE1 at the mRNA level at 24 h post ML141 injection. Shrimp injected with the same amount of DMSO in each group were used as controls.
|
|
S5244 |
Zoledronic acid monohydrateZoledronic acid (Zoledronate, CGP-4244) monohydrate 是 Zoledronic acid (唑来膦酸) 的一水合物,是有效的破骨细胞抑制剂,可通过抑制甲戊二羟酸途径的酶、阻止小GTP结合蛋白如Ras和Rho的异戊二烯化来诱导破骨细胞凋亡。 |
||
S6752 |
Y16Y16是G蛋白偶联Rho GEFs抑制剂。它能阻止LARG和Rho的结合,Kd值为80 nM。 |
目录号 | 产品描述 | 文献引用 | 实验数据 |
---|---|---|---|
S0765New |
MAZ51MAZ51 是一种选择性的 vascular endothelial growth factor receptor (VEGFR)-3 (Flt-4) tyrosine kinase 的有效抑制剂。MAZ51 通过 Akt/GSK3β 的磷酸化和 RhoA 的激活来诱导神经胶质瘤细胞的细胞圆缩和G2/M细胞周期停滞。 MAZ51 可抑制多种非VEGFR-3表达肿瘤细胞的增殖并诱导其凋亡。 |